Thrombolytics

Question 1

PKs of aspirin

Answer 1

Inhibits Thromboxane A2 formation by inhibiting cyclooxygenase

Also inhibits prostacyclin made by vascular endothelium

Question 2

Discuss Dipyridamole

Answer 2

Vasodilator and inhibitor of platelet aggregation by stopping phosphodiesterase

Question 3

Name the platelet ADP receptor inhibitors

Answer 3

Clopidogrel, Prasugrel, Ticagrelor, Cangrelor

Question 4

PKs of Clopidgrel

Answer 4

1. Thienopyridine prodrug that blocks (irreversibly) G1 coupled ADP receptor P2Y12
2. DDIs with PPIs
3. Can cause GI bleeds
4. Requires CYP2C19 for activation

Question 5

PKs of Prasugrel

Answer 5

1. Same type of prodrug as Clopidgrel but doesn’t require CYP2C19 for activation

Question 6

Discuss Ticagrelor

Answer 6

1. Binds reversibly to P2Y1P ADP receptors

Question 7

Discuss Cangrelor

Answer 7

1. An ATP analog that binds reversibly to P2Y12 receptors to stop platelet aggregation
2. Given IV w/ very quick onset (2 minutes)

Question 8

Discuss Vorapaxar

Answer 8

1. PAR-1 antagonist

2. 8 day half life

Question 9

Name the glycoprotein 2b and 3a inhibitors

Answer 9

Abciximab, Eptifibatide, Tirofiban

blocks receptor for fibrinogen and vWF

Question 10

Discuss Tirofiban and Epifibatide

Answer 10

Epifibatide: derived from rattlesnake venom; reversible

Tirofiban: peptidomimetic inhibitor; reversible

Question 11

Name the Thrombolytic agents

Answer 11

Streptokinase, Alteplase tPa, Reteplase, Tenecteplase

These agents activate plasminogen